Active substanceExametasimExametasim
Similar drugsTo uncover
  • Teoksim, 99mTc
    lyophilizate in / in 
    DIAMED, LLC     Russia
  • Ceretec®
    lyophilizate in / in 
    JI Halskea Limited     United Kingdom
  • Dosage form: & nbsplyophilizate for the preparation of a solution for intravenous administration
    Composition:

    1 bottle with lyophilizate contains:

    Active substance: Exametasim - 0.5 mg

    Excipients:

    Sodium chloride 4.5 mg

    Tin dichloride dihydrate 7.6 μg

    1 ml of the finished product contains:

    Active substance: Exametasim - 0.1 mg

    99mTc -74-222 MBq

    Excipients:

    aboutfishing dichloride dihydrate 1.5 μg, which corresponds

    tin dichloride and tin tetrachloride 0,78 mkg

    Sodium chloride 9.9 mg

    Water for injections up to 1 ml

    Description:

    The lyophilizate is white or almost white in color.

    The finished product is a colorless transparent liquid, free of mechanical inclusions.

    Pharmacotherapeutic group:Radiopharmaceutical diagnostic tool, central nervous system, radiopharmaceutical diagnostic tool, visualization of inflammation and its localization.
    ATX: & nbsp

    V.09.A.A.01   99m Tc-Technetium-exametazime

    Pharmacodynamics:

    Ceretec® is a lyophilizate used to prepare a diagnostic radiopharmaceutical by dissolving it in a sodium solution 99mTc-pertechnetate obtained from a generator 99mTc. Isotope 99mTc has a half-life of 6 hours, during the decay emits gamma quanta with an energy of 140 KeV and a yield of 90%.

    Pharmacological effects after intravenous administration of Cereketo in the recommended doses are not noted.

    Pharmacokinetics:

    Intravenous administration

    99mTc-eksemetazim is a non-polar lipophilic complex, which has a low molecular weight and is able to penetrate the blood-brain barrier. After intravenous administration, the drug is rapidly excreted from the blood. The content of the drug in the brain reaches a maximum of 3.5-7.0 % from the administered dose within one minute after intravenous administration. About 15% of the dose accumulated in the brain is washed out to the 2nd minute after the injection, after which the level of the drug slowly changes within 24 hours mainly in connection with the decay process 99mTc. The drug is distributed in the brain, as well as in muscles and soft tissues. About 20 % The administered dose is detected in the liver immediately after injection and is excreted from it with bile. About 40% of the administered dose is excreted by the kidneys with urine within 48 hours after administration, which is accompanied by a significant decrease in the concentration of the drug in skeletal muscles and soft tissues.

    Labeled white blood cells

    Autologous leukocytes, labeled 99mTc-eksemetazimom in vitro, with the subsequent introduction into the bloodstream are a non-invasive way to diagnose various inflammatory conditions, as a result of natural migration of leukocytes to the inflammatory foci. After separation of leukocytes and introduction of a label into them, the labeling efficiency is determined, equal to approximately 55%, of which, about 78% is associated with neutrophils.

    After injection into the bloodstream, leukocytes labeled 99mTc in vitro, distributed in the liver (within 5 minutes) and the spleen (for about 40 minutes) and in the general circulation (the latter represents about 50% of the total number of white blood cells).

    Approximately 37% of leukocytes labeled 99mTc, is released from the bloodstream 40 minutes after the injection. Activity 99mTc is gradually decreasing and excreted partly by the kidneys, partly by the liver and through the gallbladder, which leads to accumulation of activity in the large intestine.

    Indications:

    CereTEC® is for diagnostic use only.

    Scintigraphy of the brain for the diagnosis of diseases associated with impaired cerebral circulation, in particular, transient cerebral ischemia, stroke, epilepsy, dementia, tumor neoplasms.

    When using labeled white blood cells - for visualization of inflammatory foci of different origin and localization.

    Contraindications:

    Hypersensitivity to exametasim or any other component of the drug.

    Pregnancy (see the section "Pregnancy and the period of breastfeeding").

    Age to 18 years, because the effectiveness and safety of use in patients of this age group are not established.

    Pregnancy and lactation:

    If it is necessary to administer radiopharmaceuticals to women of childbearing age, it is necessary to obtain reliable information about the absence of pregnancy. Any woman who has a delay in menstruation should be considered pregnant until the opposite is proven. Consider using alternative methods that do not use ionizing radiation.

    The drug should not be used in pregnant women, except when the intended benefit to the mother from its use exceeds the potential risk to the fetus.

    Data on excretion 99mTc-exometasim in breast milk is absent; if the introduction of a radiopharmaceutical is necessary for the patient during breastfeeding,It should be recommended that she stop breastfeeding for at least 24 hours after drug administration.

    Dosing and Administration:

    Ready-to-use drug is administered intravenously.

    Preparing the preparation

    All operations should be performed in compliance with aseptic methods.

    1. Place the vial with lyophilisate in a protective container and remove the protective cap.

    2. Wipe the vial stopper with a tissue for disinfection.

    3. Using a 10 ml sterile syringe with protection from ionizing radiation, add 99t in a vial of lyophilizate 5 ml sterile eluate from the generator 99mTc (see the "Recommendations").

    4. Before you remove the syringe from the vial with the drug, you need to get into it 5 ml of gas above the solution to normalize the pressure inside the vial.

    5. Gently shake the bottle for 10 seconds until the lyophilizate is completely dissolved.

    6. Determine the total radioactivity in the vial and calculate the volume required for administration to the patient or for the preparation of labeled 99mTc of leukocytes.

    7. Radioactivity, volume, date and time of preparation to write down on a sticker for a vial.

    8. Cook the prepared preparation for 30 minutes after preparation.

    9. Dispose of any unused radioactive material in accordance with the established requirements.

    Recommendations

    To achieve maximum radiochemical purity in the preparation of the solution, a fresh eluate obtained less than 2 hours before the solution is prepared from 99mTc generator, which was eluted for 24 hours.

    You can add 0.37 - 1.11 GBq (10 - 30 mCi) to the vial 99mTc.

    Before preparing the solution, the eluate can be brought to the required concentration of radioactivity (0.37-1.11 GBq in 5 ml) by dilution with saline for injection chloride.

    The pH of the prepared solution for injection should be within 9.0 - 9.8. Scintigraphy of the brain

    The recommended activity is 350 - 500 MBq.

    Localization of the centers of accumulation of leukocytes, labeled 99tTc in vivo

    The recommended activity is 200 MBq.

    A suspension of leukocytes labeled 99mTc, injected with a needle 19G in the shortest possible time after its preparation. In dynamic mode, visualization can be carried out within the first 60 minutes after the introduction of the suspension to determine the clearance of the lungs and for visualization of cell migration.Static visualization should be performed 3-4 hours later and 24 hours after the introduction of the suspension to detect focal hyper-fixation of leukocytes.

    Radiation loads

    Scintigraphy of the brain

    The table presents dosimetry data according to publication No. 62 of the International Commission on Radiological Protection (ICRP), Pergamon Press, 1991.

    Organ target

    The absorbed dose per unit of injected activity (mGy / MBq)

    Adrenal glands

    5, ЗЕ-03

    The wall of the bladder

    2, ЗЕ-02

    Surface of bones

    5,1Е-03

    Brain

    6,8Е-03

    Breast

    2,0Е-03

    Gallbladder

    1.8E-02

    Gastrointestinal tract


    The wall of the stomach

    6.4E-03

    Small intestine

    1,2Е-02

    The wall of the upper parts of the thick

    1.8E-02

    intestines


    The wall of the lower parts of the thick

    1,5Е-02

    intestines


    A heart

    3,7E-03

    Kidneys

    3,4E-02

    Liver

    8,6Е-03

    Lungs

    ЩЕ-02

    Muscles

    2,8Е-03

    Esophagus

    2,6Е-03

    Ovaries

    6,6Е-03

    Pancreas

    5DE-03

    Red marrow

    3,4Е-03

    Leather

    1,6Е-03

    Spleen

    4, ЗЕ-03

    Eggs

    2,4Е-03

    Thymus

    2,6Е-03

    Thyroid

    2,6Е-02

    Uterus

    6,6Е-03

    Other bodies

    3,2Е-03

    The effective equivalent dose (mSv / MBq)

    9, ЗЕ-03

    The effective dose is 4.7 mSv / 500 mBq, calculated per adult patient (70 kg).

    Scintigraphy of foci of inflammation

    The table presents dosimetry data in accordance with the publication No. 80 of the International Commission on Radiological Protection (ICRP), radiation doses for patients after receiving a radiopharmaceutical, Pergamon Press, 1998.

    Organ

    Absorbed dose per unit of injected activity

    (mGy / MBq)


    Adults

    15 years

    10 years

    5 years

    1 year


    Adrenal glands

    1.0Е-02

    1.2Е-02

    1.8Е-02

    2.6Е-02

    4.3E-02


    The wall of the bladder

    2.6Е-03

    3.5Е-03

    5.2Е-03

    7.8Е-03

    1.4Е-02


    Surface of bones

    K6E-02

    2LE-02

    3.4E-02

    6LE-02

    K5E-01


    Brain

    2.3Е-03

    2.9Е-03

    4.4Е-03

    7.0E-03

    1.3Е-02

    Breast

    2.4Е-03

    2.9Е-03

    4.9Е-03

    7.6E-03

    1.3Е-02

    Gallbladder

    8.4E-03

    1.0Е-02

    1.6Е-02

    2,5Е-02

    3.6Е-02

    Gastrointestinal tract






    The wall of the stomach

    8LE-03

    9.6Е-03

    1.4Е-02

    2DE-02

    3,2Е-02

    Small intestine

    4,6Е-03

    5,7Е-03

    8JE-03

    TZE-02

    2.1 E-02

    Colon

    4.3E-03

    5.4Е-03

    8D-E-03

    K2E-02

    2 Л Е-02

    The wall of the upper divisions of the large intestine

    4,7Е-03

    5,9Е-03

    9, ЗЕ-03

    1,4Е-02

    2, ЗЕ-02

    The wall of the lower parts of the large intestine

    3,7E-03

    4,8Е-03

    7, ZE-03

    1,0Е-02

    1.8E-02

    A heart

    9.4E-03

    1.2Е-02

    1.7Е-02

    2.5E-02

    4.4E-02

    Kidneys

    1.2Е-02

    1.4Е-02

    2.2E-02

    3,2Е-02

    5.4Е-02

    Liver

    2.0Е-02

    2.6Е-02

    3.8E-02

    5.4Е-02

    9JE-02

    Lungs

    7.8Е-03

    9,9Е-03

    1.5Е-02

    2.3E-02

    4 L Е-02

    Muscles

    ZZE-OZ

    4.1Е-03

    6.0Е-03

    8.9Е-03

    K6E-02

    Esophagus

    3,5Е-03

    4,2Е-03

    5.8Е-03

    8.6Е-03

    1.5Е-02

    Ovaries

    3,9Е-03

    5,0Е-03

    7,2Е-03

    1,1E-02

    T8E-02

    Pancreas

    1, ЗЕ-02

    1,6E-02

    2, ЗЕ-02

    3,4E-02

    5, ЗЕ-02

    Red marrow

    2, ЗЕ-02

    2,5Е-02

    4,0Е-02

    7.1 E-02

    1.4Е-01

    Leather

    1.8Е-03

    2.1 E-03

    3.4Е-03

    5.5Е-03

    1.0Е-02

    Spleen

    T5E-01

    2.1Е-01

    ZLE-01

    4.8Е-01

    8.5Е-01

    Eggs

    1,6Е-03

    2L E-03

    3,2Е-03

    5 L Е-03

    9.2Е-03

    Thymus

    3.5Е-03

    4.2Е-03

    5,8Е-03

    8.6Е-03

    K5E-02

    Thyroid

    2.9Е-03

    3.7Е-03

    5.8Е-03

    9.3Е-03

    T7E-02

    Uterus

    3.4Е-03

    4.3E-03

    6.5Е-03

    9.7E-03

    K6E-02

    Other bodies

    3.4Е-03

    4.2Е-03

    6.3Е-03

    9.5Е-03

    K6E-02

    The effective equivalent dose (mSv / MBq)

    1DE-02

    1,4Е-02

    2.2E-02

    3,4E-02

    6,2Е-02










    The effective dose is 2.2 mSv / 200 MBq per adult patient (70 kg).

    Side effects:

    Adverse effects when administered 99mTc-eksaksamazima are very rare: reported on the development of reactions of hypersensitivity, accompanied by the appearance of a rash after intravenous injection of the finished product. Also, a possible development of a hypersensitivity reaction after administration of leukocytes labeled 99mTc in vivo. For each patient, the effects of ionizing radiation should be justified in view of the expected positive effect. The radioactivity of the injected preparation should be such that the final radiation is as low as possible, taking into account the need to obtain the required diagnostic result. The effect of radiation can be associated with the development of cancer and the possibility of the appearance of inherited defects. According to the currently available data for diagnostic radiation studies, such negative effects are unlikely because of the low radiation dose.For most diagnostic radiation studies, the dose received does not exceed 20 mSv. In some studies, doses can be adjusted upwards.

    System of organs

    Frequency*

    Undesirable reactions

    Infringements from

    it is not known

    Hypersensitivity, including

    immune system


    rash, erythema, urticaria,



    angioedema, itching


    not known (only

    Hypersensitivity, including


    for introduction

    rash, erythema, urticaria,


    labeled

    angioedema, itching,


    leukocytes)

    anaphylactoid reaction or



    anaphylactoid shock

    Infringements from

    it is not known

    headache, dizziness,

    nervous system


    paresthesia

    Infringements from

    it is not known

    tides

    vessels



    Infringements from

    it is not known

    nausea, vomiting

    gastrointestinal



    tract



    General disorders and

    it is not known

    asthenia (for example, weakness,

    changes in place


    fatigue)

    injections



    * very often: incidence of complication -> or = 10%;

    often: the incidence of complications -> or = 1%, <10%;

    not often: frequency of occurrence of complication -> or = 0,1%, <1 %;

    rarely: incidence of complication -> or = 0.01%, <0.1%;

    very rarely: frequency of occurrence - <0.01%;

    It is not known: the frequency can not be calculated on the basis of available data.

    Overdose:

    When using the drug in accordance with the instructions for medical use, an overdose is unlikely. In case of an overdose, frequent urination and defecation should be stimulated to reduce the radiation burden on the patient.

    Interaction:

    Not found. It is not recommended to mix the drug with other medicines.

    Special instructions:

    The vial with lyophilizate contains 1.77 mg of sodium / vial (0.354 mg / ml), which should be taken into account in patients who are on a hyponatrial diet.

    The use of the drug may cause hypersensitivity reactions, including anaphylaxis. In case of their occurrence, it is necessary to have the necessary drugs and equipment for immediate medical care.

    The preparation should be prepared and applied only by qualified personnel in the department of nuclear medicine in conditions asepsis. The introduction of radiopharmaceuticals creates risks of external radiation contamination with urine, vomit, etc.Precautions should be observed when working with radioactive materials, as well as the conditions for aseptic work with the drug. The finished product is stored in accordance with national rules for ensuring radiation safety. Any unused radioactive material is disposed of in accordance with applicable law.

    Before using the drug, to confirm the quality, it is necessary to determine the radiochemical purity of the drug according to the following procedure:

    Determination of radiochemical purity

    In the prepared solution of exometasim for injection, three potential impurities may be present. This is a secondary complex 99mTc-eksametazima, free pertechnetate and reduced-hydrolyzed 99mTc. To fully determine the radiochemical purity of the drug solution, two chromatographic systems should be used: butane-2-one (MEK) and 0.9% sodium chloride solution.

    The samples of the test solution are applied with a needle about 2.5 cm from the lower edge of the two chromatographic strips Varian SA (2 cm (± 2 mm) x 20 cm). After that, the strips are immediately placed in the prepared chromatographic chambers, which contain a fresh solvent with a layer thickness of 1 cm, for ascending chromatography.After moving solvent front to 14 cm from the start, the strip is removed from the chromatographic chamber, dried and radioactivity was determined using suitable equipment.

    Chromatography results System 1 (Varian SA: Butan-2-one (MEK)

    Secondary complex 99mTc-eksametazima and reduced-hydrolyzed 99mTc remain on the sample line.

    Lipophilic complex 99mTc-eksametazima and pertechnetate move with the front (Rf 0,8-1,0).

    System 2 (Varian SA: 0.9% sodium chloride)

    Lipophilic complex 99mTc -exexametasim, secondary complex 99mTc-eksemetazim and

    reconstituted-hydrolyzed 99mTc remain at the start.

    Pertechnetat moves with Rf 0,8-1,0.

    Calculate the activity (%) due to the complex 99mTc -exexamazime and reduced-hydrolyzed 99mTc on the chromatograms of System 1 (A%). Calculate the activity (%) due to pertechnetate according to System 2 chromatograms (B%). Radiochemical purity (as a percentage of the lipophilic complex 99m-eksametazima are defined as follows: 100 - (% A +% B), where A% - level secondary complex 99mTc -exexametam and reconstituted-hydrolyzed 99mTc; In% - the level of pertechnetate.

    When sampling for the test within 30 minutes after preparation of the drug solution, it can be expected that the radiochemical purity will be at least 80%. The test for determination of radiochemical purity should be carried out immediately after sampling.

    The procedure for the isolation of leukocytes and their subsequent labeling in vitro 99mTc-exometasim

    All operations should be performed in compliance with aseptic methods.

    1. In two 60 ml plastic non-heparinized syringe, dial 9 ml of a mixture consisting of a solution of citric acid - dextrose citrate (see "Notes").

    2. In each of the syringes, using a butterfly needle (19G), select 51 ml of blood from the patient. Close the syringes with sterile tips.

    3. Prepare 5 universal tubes and add 2 ml of hydroxyethyl starch solution.

    4. Without inserting the needle into the syringe, transfer 20 ml of blood from the syringes to each of the 5 universal tubes containing hydroxyethyl starch. The remaining 20 ml of blood is transferred to a tube that does not contain hydroxyethyl starch.

    Recommendation: to prevent the formation of bubbles and foaming, the blood should be carefully drained over the walls of the test tubes.

    5. Gently mix blood and hydroxyethyl starch by a single overturning of the test tube. Remove the cap from the universal tube and remove any air bubbles with a sterile needle. Put on the lid and allow the tubes to settle for 30-60 minutes to settle the red blood cells.

    Recommendation: the rate of erythrocyte sedimentation depends on the patient's state of health. The process can be considered complete when the red blood cells settle at least half of the entire volume of the tube.

    6. In parallel, a second tube, free from hydroxyethyl starch and containing 20 ml of whole blood, is centrifuged at 2000 g within 10 minutes. The resulting supernatant contains a cell-free plasma and a citric acid solution, dextrose citrate, and stored at room temperature. The supernatant is used as an environment for labeling leukocytes.

    7. After the completion of the process of precipitation of erythrocytes in the first tube, carefully, avoiding the entry of red blood cells, transfer 15 ml of supernatant (turbid liquid of pale yellow color), consisting of plasma with leukocytes and platelets, into pure universal test tubes.

    Recommendation: When sampling, do not use the needle to avoid accidental cell damage.

    8. The resulting supernatant is centrifuged at 150 g for 5 minutes to obtain a supernatant consisting of plasma with platelets, and a sediment - a "mixture" of leukocytes.

    9. The maximum possible amount of supernatant is transferred to clean universal tubes and centrifuged at 2000g for 10 minutes to obtain an additional supernatant fluid free of plasma cells. The resulting supernatant contains hydroxyethyl starch and will be used to wash the cells after inserting a label in them.

    10. In parallel, gently tapping and rotating the tube, detach from the walls sediment, which is a "mixture" of leukocytes. A syringe without a needle, put the cells in one tube and, using the same syringe, add 1 ml of the supernatant obtained in step 6. Gently rotating the tube, resuspend the cells.

    11. Using the procedure described in the paragraph "Preparing the preparation," prepare a solution 99mTc-eksametazima, by adding from the generator 99mTc 5 ml eluate with content 99mTc O4-500 MBq (13.5 mCi).

    12. Immediately add 4 ml of the prepared solution 99mTc-eksametazima in the "mixture" of leukocytes and supernatant (see item 10).

    13. Caution Rotate the tube, mix the contents and leave for 10 minutes at room temperature.

    14. If necessary, immediately apply the samples to chromatographic strips for the assessment of radiochemical purity 99mTc-exometasim according to the instructions set forth in the paragraph "Determination of radiochemical purity".

    15. In order to stop the process of introducing labels into the cells, after 10 minutes in a test tube Caution add 10 ml of supernatant (see point 9), cell-free and containing hydroxyethyl starch. Mix the contents of the tube with a gentle rotational motion.

    16. Centrifuge at 150 g within 5 minutes.

    17. Select and store the supernatant.

    Recommendation. It is necessary that at this stage the entire supernatant containing unbound 99mTc-eksametazim, was maximally completely taken from the tube, for which a needle with a wide channel is used.

    18. Rotating gently for mixing, resuspend the leukocyte mixture, QQ labeled 99mTc, in 5-10 ml of the supernatant obtained in step 6.

    19. Measure the radioactivity of cells and supernatant from point 17.Calculate the efficiency of the labeling process in percent, which is defined as the ratio of activity in cells to the sum of activities in cells and supernatant.

    Recommendations. The effectiveness of the labeling process depends on the number of leukocytes in the patient and varies depending on the volume of the sample of the selected blood. When using the volumes specified in clause 2, the expected effectiveness of the labeling process [LE] will be about 55%.

    20. With a syringe without a needle, gently take the labeled cells into a plastic, non-heparinized syringe and close it with a sterile cap. Measure radioactivity.

    21. After this, the labeled cells are ready for administration, which should be carried out without delay.

    Notes: To prepare 1 liter of a mixture of a solution of citric acid - dextrose citrate, you should transfer 22 g of trisodium citrate, 8 g of citric acid, 22.4 g of dextrose to a graduated flask and bring the volume of water for injection to 1.0 liters. All operations should be performed in compliance with aseptic methods. Sterilize by filtration through a Millipore filter (0.2 μm). Store at room temperature.It is allowed to use a ready-made industrial solution, which must be stored in accordance with the manufacturer's recommended conditions and used before the expiration date.

    Preparation of 6% hydroxyethyl starch should also be carried out in accordance with aseptic methods. It is allowed to use a ready-made industrial solution, which must be stored in accordance with the manufacturer's recommended conditions and used before the expiration date.

    It is important that the labeled leukocytes are thoroughly washed before being administered to the patient.

    Effect on the ability to drive transp. cf. and fur:

    The effect of using the drug on the ability to drive vehicles, as well as machines and mechanisms when applying it in accordance with the instruction for medical use, has not been established.

    Form release / dosage:

    2 mg of lyophilizate for the preparation of a solution for intravenous administration

    Packaging:

    In a colorless transparent bottle (Hebrew Farm, Type I) with a capacity of 10 ml, closed with a plug of chlorobutyl rubber and crimped with an aluminum cap with a snap-off plastic lid.

    For 2 or 5 bottles complete with stickers (2 or 5) and instructions for medical use are placed in a cardboard box.

    Storage conditions:

    Lyophilizate: Store at a temperature of no higher than 25 ° C, do not freeze. Keep out of the reach of children.

    Ready-to-use drug: Store at 15-25 ° C, do not freeze. Store in accordance with national requirements for radiation safety.

    Shelf life:

    Lyophilizate - 52 weeks from the date of manufacture.

    Ready to use the drug within 30 minutes from the time of preparation.

    Do not use after expiry date.

    Terms of leave from pharmacies:For hospitals
    Registration number:П N016296 / 01
    Date of registration:27.09.2011
    The owner of the registration certificate:JI Halskea LimitedJI Halskea Limited United Kingdom
    Manufacturer: & nbsp
    JI Halskea Limited United Kingdom
    Representation: & nbspJI Halskea Nycomed Distribution Ltd.JI Halskea Nycomed Distribution Ltd.Russia
    Information update date: & nbsp20.10.2015
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